ChEMBL ligand: CHEMBL3728620
PAR4/Proteinase activated receptor 4 in Human [ChEMBL: CHEMBL4691] [GtoPdb: 350] [UniProtKB: Q96RI0] There should be some charts here, you may need to enable JavaScript!

DB	Assay description	Assay Type	Standard value	Standard parameter	Original value	Original units	Original parameter	Reference
PAR4/Proteinase activated receptor 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4691] [GtoPdb: 350] [UniProtKB: Q96RI0]
ChEMBL	Displacement of [3H]BMS-986120 from His-tagged human PAR4 expressed in HEK293 cell membranes	B	8.52	pKd	3	nM	Kd	J Med Chem (2019) 62: 7400-7416 [PMID:31246024]
ChEMBL	Displacement of [3H]BMS-986120 from His-tagged human PAR4 expressed in HEK293 cell membranes measured after 2 hrs	B	8.85	pKd	1.4	nM	Kd	J Med Chem (2019) 62: 7400-7416 [PMID:31246024]
ChEMBL	Antagonist activity at PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation preincubated for 5 mins followed by gamma-thrombin addition and measured in presence of recombinant hirudin	B	7.6	pIC50	25	nM	IC50	J Med Chem (2019) 62: 7400-7416 [PMID:31246024]
ChEMBL	Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay	F	7.61	pIC50	24.74	nM	IC50	WO-2013163244-A1. Imidazothiadiazole derivatives as protease activated receptor 4 (PAR4) inhibitors for treating platelet aggregation (2013)
ChEMBL	Antagonist activity at PAR4 in human washed platelets assessed as inhibition of gamma-thrombin-induced platelet aggregation preincubated for 5 mins followed by gamma-thrombin addition and measured every 50 secs for up to 15 mins starting from 10 secs post gamma-thrombin addition in presence of recombinant hirudin	B	8.1	pIC50	8	nM	IC50	J Med Chem (2019) 62: 7400-7416 [PMID:31246024]
ChEMBL	Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay	F	8.62	pIC50	2.42	nM	IC50	WO-2013163244-A1. Imidazothiadiazole derivatives as protease activated receptor 4 (PAR4) inhibitors for treating platelet aggregation (2013)
ChEMBL	Antagonist activity at full-length human PAR4 expressed in HEK293 cells assessed as inhibition of AYPGKF-induced intracellular calcium mobilization preincubated for 30 mins followed by AYPGKF addition and measured by calcium indicator-based FLIPR assay	F	8.62	pIC50	2.4	nM	IC50	J Med Chem (2019) 62: 7400-7416 [PMID:31246024]
GtoPdb	Measuring inhibition of PAR4 agonist-induced intracellular calcium mobilization in HEK293-PAR4 cells by FLIPR assay.	-	8.62	pIC50	2.4	nM	IC50	J Med Chem (2019) 62: 7400-7416 [PMID:31246024]

ChEMBL data shown on this page come from version 33:

Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]